Design and synthesis of HIV-1 protease inhibitors. Novel tetrahydrofuran P2/P2'-groups interacting with Asp29/30 of the HIV-1 protease. Determination of binding from X-ray crystal structure of inhibitor protease complex.

Oscarsson K; Lahmann M; Lindberg J; Kangasmetsa J; Unge T; Oscarson S; Hallberg A; Samuelsson B

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Design and synthesis of HIV-1 protease inhibitors. Novel tetrahydrofuran P2/P2'-groups interacting with Asp29/30 of the HIV-1 protease. Determination of binding from X-ray crystal structure of inhibitor protease complex.

机译：HIV-1蛋白酶抑制剂的设计和合成。新型四氢呋喃P2 / P2'-基团与HIV-1蛋白酶的Asp29 / 30相互作用。从抑制剂蛋白酶复合物的X射线晶体结构确定结合。

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A series of HIV-1 protease inhibitors having new tetrahydrofuran P2/P2' groups have been synthesised and tested for protease inhibition and antiviral activity. Six novel 4-aminotetrahydrofuran derivatives were prepared starting from commercially available isopropylidene-alpha-D-xylofuranose yielding six symmetrical and six unsymmetrical inhibitors. Promising sub nanomolar HIV-1 protease inhibitory activities were obtained. The X-ray crystal structure of the most potent inhibitor (23, K(i) 0.25 nM) co-crystallised with HIV-1 protease is discussed and the binding compared with inhibitors 1a and 1b.

机译：已合成了一系列具有新的四氢呋喃P2 / P2'基团的HIV-1蛋白酶抑制剂，并测试了其蛋白酶抑制作用和抗病毒活性。从市售的异亚丙基-α-D-木呋喃糖开始制备了六种新颖的4-氨基四氢呋喃衍生物，产生了六种对称和六种不对称抑制剂。获得了有希望的亚纳摩尔HIV-1蛋白酶抑制活性。讨论了与HIV-1蛋白酶共结晶的最有效抑制剂（23，K（i）0.25 nM）的X射线晶体结构，并与抑制剂1a和1b进行了比较。

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《Bioorganic and medicinal chemistry》 |2003年第6期|共9页
作者
Oscarsson K; Lahmann M; Lindberg J; Kangasmetsa J; Unge T; Oscarson S; Hallberg A; Samuelsson B;
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正文语种 eng
中图分类药学;生物化学;
关键词
HIV-1; Endopeptidases; Protease Inhibitors; structure; binding; 蛋白酶抑制药;

机译：HIV-1;Endopeptidases;Protease Inhibitors;structure;binding;蛋白酶抑制药;

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1. Design and synthesis of HIV-1 protease inhibitors. Novel tetrahydrofuran P2/P2'-groups interacting with Asp29/30 of the HIV-1 protease. Determination of binding from X-ray crystal structure of inhibitor protease complex. [J] . Oscarsson K, Lahmann M, Lindberg J, Bioorganic and medicinal chemistry . 2003,第6期

机译：HIV-1蛋白酶抑制剂的设计和合成。新型四氢呋喃P2 / P2'-基团与HIV-1蛋白酶的Asp29 / 30相互作用。从抑制剂蛋白酶复合物的X射线晶体结构确定结合。
2. Design and Synthesis of Potent HIV-1 Protease Inhibitors Containing Bicyclic Oxazolidinone Scaffold as the P2 Ligands: Structure-Activity Studies and Biological and X-ray Structural Studies [J] . Ghosh Arun K., Williams Jacqueline N., Ho Rachel Y., Journal of Medicinal Chemistry . 2018,第21期

机译：含有双环恶唑烷酮支架作为P2配体的强化HIV-1蛋白酶抑制剂的设计与合成：结构 - 活性研究和生物学和X射线结构研究
3. Design and Synthesis of Highly Potent HIV-1 Protease Inhibitors Containing Tricyclic Fused Ring Systems as Novel P2 Ligands: Structure-Activity Studies, Biological and X-ray Structural Analysis [J] . Ghosh Arun K., Nyalapatla Prasanth R., Kovela Satish, Journal of Medicinal Chemistry . 2018,第10期

机译：高效HIV-1蛋白酶抑制剂的设计与合成含有三环熔环系统作为新型P2配体：结构 - 活性研究，生物学和X射线结构分析
4. Coarse-Grained Modeling of the HIV-1 Protease Binding Mechanisms: I. Targeting Structural Flexibility of the Protease Flaps and Implications for Drug Design [C] . Gennady M. Verkhivker International Meeting on Computational Intelligence Methods for Bioinformatics and Biostatistics . 2009

机译：HIV-1蛋白酶结合机制的粗粒模型：I.靶向蛋白酶襟翼的结构柔韧性和对药物设计的影响
5. Asymmetric synthesis of bis-tetrahydrofuran and its conversion to darunavir and design of novel HIV-1 protease inhibitors based upon the 'backbone binding concept'. [D] . Yashchuk, Sofiya. 2010

机译：双-四氢呋喃的不对称合成及其向darunavir的转化以及基于“骨干结合概念”的新型HIV-1蛋白酶抑制剂的设计。
6. Design synthesis X-ray studies and biological evaluation of novel macrocyclic HIV-1 protease inhibitors involving the P1′–P2′ ligands [O] . Arun K. Ghosh, W. Sean Fyvie, Margherita Brindisi, -1

机译：设计合成X射线研究和涉及P1–P2配体的新型大环HIV-1蛋白酶抑制剂的生物学评估
7. Design ofgem-Difluoro-bis-Tetrahydrofuran as P2 Ligand for HIV-1 Protease Inhibitors to Improve Brain Penetration: Synthesis, X-ray Studies, and Biological Evaluation [O] . Arun K. Ghosh, Sofiya Yashchuk, Akira Mizuno, 2014

机译：设计OFGEM-DIFLUORO-BIS-四氢呋喃作为HIV-1蛋白酶抑制剂的P2配体，提高脑渗透：合成，X射线研究和生物学评估

Design and synthesis of HIV-1 protease inhibitors. Novel tetrahydrofuran P2/P2'-groups interacting with Asp29/30 of the HIV-1 protease. Determination of binding from X-ray crystal structure of inhibitor protease complex.

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